SEP 24, 2014 05:00 AM PDT

Exploring macrocycles for drug discovery: Novel lead series for challenging protein-protein interactions

Speakers
  • Chief Scientific Officer, Ensemble Therapeutics
    Biography

       
      Nick joined Ensemble Therapeutics as the Chief Scientific Officer in May 2006. In his role as CSO, Nick heads up the firm's drug discovery program investigating the rapid synthesis of macrocycles using DNA-programmed chemistry, as drug candidates for disease relevant protein-protein and protease targets.After working as a medicinal chemist for Glaxo, Nick joined Pfizer in Sandwich, England in 1984. He worked initially in cardiovascular disease, and is an inventor on patents for the neutral endopeptidase inhibitor candoxatrilat. Later he led the chemistry team on cGMP PDE inhibitors for angina and erectile dysfunction, and is an inventor on patents for Viagra. Subsequently, Nick established Pfizer's combinatorial chemistry group and authored several related papers and a textbook. He also managed the high throughput screening group and materials management, and played a key role in the global integration of the Pfizer, Warner-Lambert and Pharmacia compound collections. In 2003 Nick moved to the Pfizer Research Technology Center in Cambridge, Massachusetts, to lead the Chemical Sciences group investigating new targets for drug discovery and new chemistry technologies.  
       
       

    Abstract:

    Macrocycles offer a new structural class that has the potential to address challenging protein-protein interaction targets and still present attractive drug-like properties including cell membrane penetration and oral bioavailability. Indeed a number of orally active drugs based on naturally occurring macrocycles provide a compelling precedent for this argument. Ensemble have used DNA-programmed chemistry to make over 10 million synthetic macrocycles in a library format that permits rapid and efficient screening against therapeutically relevant targets. The talk will present successful Ensemble case studies with XIAP antagonists for oncology, and IL17 antagonists for inflammatory disease.


    Show Resources
    You May Also Like
    SEP 05, 2019 04:00 PM CEST
    C.E. CREDITS
    SEP 05, 2019 04:00 PM CEST
    DATE: September 5, 2019TIME: 7:00am PT, 10:00am ET, 4:00pm CEST PCR (Polymerase Chain Reaction) has gone through a massive evolution since its development in 1983. Besides it...
    MAY 16, 2019 04:00 PM CEST
    C.E. CREDITS
    MAY 16, 2019 04:00 PM CEST
    DATE: May 16, 2019TIME: 7:00am PDT, 10:00am EDT, 4:00pm CEST The emergence of NGS is revolutionizing the microbiological sciences and transforming medicine. Deep sequencing has...
    AUG 27, 2019 09:00 AM PDT
    C.E. CREDITS
    AUG 27, 2019 09:00 AM PDT
    DATE: August 27, 2019 TIME: 9:00am PDT, 12:00pm EDT Immunotherapies targeting PD-1 or PD-L1 have proven remarkably effective for treating cancer in some patients, with considerabl...
    JUN 19, 2019 10:00 AM PDT
    JUN 19, 2019 10:00 AM PDT
    DATE: June 19, 2019TIME: 10:00am PDT, 1:00pm EDT As we develop new methods to create more biologically relevant models for research in understanding disease etiology and in...
    OCT 02, 2019 11:00 AM PDT
    OCT 02, 2019 11:00 AM PDT
    DATE: October 2, 2019TIME: 11:00am PDT, 2:00pm EDT Ditch the Excel spreadsheets and manage your molecular workflows entirely in your LIMS Achieve configuration of molecular workf...
    AUG 15, 2019 09:00 AM PDT
    C.E. CREDITS
    AUG 15, 2019 09:00 AM PDT
    DATE: August 15, 2019TIME: 9:00am PDT, 12:00pm EDT Radiation therapy is a critical tool for the treatment of brain tumors, however, exposure to high doses of ionizing radiation...
    Loading Comments...
    Show Resources